A novel peptide for efficient siRNA delivery in vitro and therapeutics in vivo. (15th July 2015)

• Record Type: Journal Article
• Authors: Pan, Ran; Xu, Wen; Yuan, Feng; Chu, Dafeng; Ding, Yong; Chen, Baoling; Jafari, Mousa; Yuan, Yongfang; Chen, P.
• Is Part Of: Acta biomaterialia. Volume 21(2015)
• Page Start: 74
• Page End: 84
• Publication Date: 2015-07-15
• Subjects: siRNA delivery -- Cell penetrating peptide -- Stearic acid -- Nuclear localization sequence -- Intratumoral injection; Biomedical materials -- Periodicals; 610.28
• DOI: 10.1016/j.actbio.2015.04.002
• Languages: English
• ISSNs: 1742-7061

Abstract

Graphical abstract: Abstract: Small interfering RNA (siRNA) shows great therapeutic potential due to its ability to regulate gene expression in a highly selective manner. However, its application has been limited by ineffective cellular uptake of siRNAs. To achieve successful gene-silencing efficiency, a safe and effective delivery vector is generally required. In this study, we designed a series of amphipathic peptides that comprised a variant of a nuclear localization sequence, 0–6 histidine residues and an optional stearic acid group. Among these candidates, STR-HK exhibited good characteristics as a safe and efficient siRNA delivery vector, facilitating efficient siRNA delivery to mammalian cells without causing cytotoxicity. Moreover, the intratumoral injection of STR-HK/siRNA complexes achieved high anti-tumor activity through the downregulation of the Bcl-2 protein in mice, with an inhibition rate of 62.8%. Our data demonstrate that STR-HK is a highly promising siRNA delivery vector for therapeutic applications.